
APG-1387
CAS No. 1570231-89-8
APG-1387( —— )
Catalog No. M21856 CAS No. 1570231-89-8
APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP).
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
5MG | 1449 | In Stock |
![]() ![]() |
10MG | 2421 | In Stock |
![]() ![]() |
100MG | Get Quote | In Stock |
![]() ![]() |
200MG | Get Quote | In Stock |
![]() ![]() |
500MG | Get Quote | In Stock |
![]() ![]() |
1G | Get Quote | In Stock |
![]() ![]() |
Biological Information
-
Product NameAPG-1387
-
NoteResearch use only, not for human use.
-
Brief DescriptionAPG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP).
-
DescriptionAPG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.
-
In VitroDasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells.Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro. Western Blot AnalysisCell Line:HepG2 and HCCLM3 cellsConcentration:0.02, 0.2, 2, 20 μM Incubation Time:1, 6, 24 hours Result:Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner.Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose.
-
In VivoDasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice.Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) monotherapy exhibits some degree of anti-tumor effect and is well tolerated in mice. Animal Model:Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells Dosage:20 mg/kg Administration:I.p. every 3 days for 4 weeks Result:Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression.Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight.
-
Synonyms——
-
PathwayApoptosis
-
TargetIAP
-
Recptor——
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number1570231-89-8
-
Formula Weight1157.4
-
Molecular FormulaC??H??N??O??S?
-
Purity>98% (HPLC)
-
SolubilityDMSO : 50 mg/mL (43.20 mM; Need ultrasonic)
-
SMILESO=S(C1=CC=CC(S(=O)(N(C[C@@H]2NC([C@@H](NC)C)=O)CC[C@](CC[C@H]3C(NC(C4=CC=CC=C4)C5=CC=CC=C5)=O)([H])N3C2=O)=O)=C1)(N(C[C@@H]6NC([C@@H](NC)C)=O)CC[C@](CC[C@H]7C(NC(C8=CC=CC=C8)C9=CC=CC=C9)=O)([H])N7C6=O)=O
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Chen Z, et, al. The SMAC Mimetic APG-1387 Sensitizes Immune-Mediated Cell Apoptosis in Hepatocellular Carcinoma. Front Pharmacol. 2018 Nov 6; 9:1298.
2. Li BX, et, al. Novel smac mimetic APG-1387 elicits ovarian cancer cell killing through TNF-alpha, Ripoptosome and autophagy mediated cell death pathway. J Exp Clin Cancer Res. 2018 Mar 12;37(1):53.
3. Li N, et, al. A novel Smac mimetic APG-1387 demonstrates potent antitumor activity in nasopharyngeal carcinoma cells by inducing apoptosis. Cancer Lett. 2016 Oct 10;381(1):14-22.
molnova catalog


